KR910004192A - Pharmaceutical composition for treating seizures containing a therapeutically effective amount of propenitoin - Google Patents

Pharmaceutical composition for treating seizures containing a therapeutically effective amount of propenitoin Download PDF

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Publication number
KR910004192A
KR910004192A KR1019900012408A KR900012408A KR910004192A KR 910004192 A KR910004192 A KR 910004192A KR 1019900012408 A KR1019900012408 A KR 1019900012408A KR 900012408 A KR900012408 A KR 900012408A KR 910004192 A KR910004192 A KR 910004192A
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KR
South Korea
Prior art keywords
composition
phosphate ester
pharmaceutical composition
prodrug
diphenylhydantoin
Prior art date
Application number
KR1019900012408A
Other languages
Korean (ko)
Inventor
알란 박서 피터
데비드 왈라스 잔
Original Assignee
로널드 에이. 다이아그놀트
워너-램버트 캄파니
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
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Application filed by 로널드 에이. 다이아그놀트, 워너-램버트 캄파니 filed Critical 로널드 에이. 다이아그놀트
Publication of KR910004192A publication Critical patent/KR910004192A/en

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/66—Phosphorus compounds
    • A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

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  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

내용 없음.No content.

Description

프로페니토인의 치료적 유효량을 함유하는 발작증 치료용 제약 조성물Pharmaceutical composition for treating seizures containing a therapeutically effective amount of propenitoin

본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음Since this is an open matter, no full text was included.

Claims (5)

단위 용량 제형의 하기 일반식(Ⅰ)의 화합물 또는 그의 제약상 허용되는 산 부가염 또는 염기 부가염, 그의 C1-C4알킬할리드 제4급 염 또는그의 N-옥시드의 치료적 유효량을 함유함을 특징으로 하는, 뇌빈혈또는 발작증 치료용 제약 조성물.A therapeutically effective amount of a compound of formula (I) or a pharmaceutically acceptable acid addition salt or base addition salt thereof, a C 1 -C 4 alkylhalide quaternary salt thereof or an N-oxide thereof in a unit dosage form A pharmaceutical composition for treating cerebral anemia or seizures, characterized in that it contains. 상기 식에서, 각각의 R은 수소 원자 또는 -CH(R1)-X-P(O)-(OH)2(여기에서 R1은 수소 원자 또는 C1-C7직쇄 또는 분지쇄 알킬기로 이루어진 군으로부터 선택되고, X는 O 또는 S임)이며, 단 R은 둘다 동시에 수소원자일 수 없다.Wherein each R is a hydrogen atom or -CH (R 1 ) -XP (O)-(OH) 2 , wherein R 1 is selected from the group consisting of a hydrogen atom or a C 1 -C 7 straight or branched alkyl group X is O or S, provided that neither R can be a hydrogen atom at the same time. 제1항에 있어서, 상기 화합물이 3-(히드록시메틸)-5,5-디페닐히단토인 포스페이트 에스테르인 조성물.The composition of claim 1 wherein said compound is phosphate ester which is 3- (hydroxymethyl) -5,5-diphenylhydanto. 제2항에 있어서, 상기 화합물이 포스페니토인 소듐 또는3-(히드록시메틸)-5,5-디페닐히단토인 포스페이트 에스테르의 디소듐 염인 조성물.The composition of claim 2 wherein said compound is sodium which is phosphenito or disodium salt of phosphate ester which is 3- (hydroxymethyl) -5,5-diphenylhydantoin. 제1항에 있어서, 상기 단위 용량 제형이 3-(히드옥시메틸)-5,5-디페닐히단토인 포스페이트 에스테르의 유리 염기 또는 그의 균등물 약 75㎎/㎖를 함유함을 특징으로 하는 조성물.The composition of claim 1, wherein said unit dose formulation contains about 75 mg / ml of a free base or equivalent thereof of 3- (hydroxyoxymethyl) -5,5-diphenylhydantoin phosphate ester. 프로드럭으로서 약 35 내지 130㎎/㎖의 3-(히드톡시메틸)-5,5-디페닐히단토인 디소듐 포스페이트 에스테르 및 pH를 약 8.3 내지 9.4로 유지시키기는데 효과적인 약 0.05 내지 2M의 완충제를 함유하며, 이때, 프로드럭은 수용액 내에서 분해되어 최소량의 페니토인과 함께 주 분해산물로서 디페닐글리신아미드를 형성하고, 상기한 pH 범위 내에서는 수용액 조성물 내의 프로드럭의 저장 수명이 최대가 되도록 분해 반응이 일어나게 됨을 특징으로 하는, 뇌빈혈 또는 발작증의 치료를 위하여 피하, 근육 또는 정맥 투여할 수 있는 안정한 제약 조성물.As a prodrug, about 35 to 130 mg / ml of 3- (hydroxythoxymethyl) -5,5-diphenylhydantoin disodium phosphate ester and about 0.05 to 2 M buffer effective to maintain pH at about 8.3 to 9.4 Wherein the prodrug is decomposed in an aqueous solution to form diphenylglycineamide as the main degradation product with a minimum amount of phenytoin, and within the pH range described above, the decomposition reaction is performed to maximize the shelf life of the prodrug in the aqueous composition. Stable pharmaceutical composition, which can be administered subcutaneously, intramuscularly or intravenously for the treatment of cerebral anemia or seizures. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.※ Note: The disclosure is based on the initial application.
KR1019900012408A 1989-08-10 1990-08-10 Pharmaceutical composition for treating seizures containing a therapeutically effective amount of propenitoin KR910004192A (en)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US39223889A 1989-08-10 1989-08-10
US392238 1989-08-10
US54107190A 1990-06-25 1990-06-25
US541.071 1990-06-25

Publications (1)

Publication Number Publication Date
KR910004192A true KR910004192A (en) 1991-03-28

Family

ID=27013811

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1019900012408A KR910004192A (en) 1989-08-10 1990-08-10 Pharmaceutical composition for treating seizures containing a therapeutically effective amount of propenitoin

Country Status (6)

Country Link
EP (1) EP0427925A3 (en)
JP (1) JP3101305B2 (en)
KR (1) KR910004192A (en)
AU (1) AU624262B2 (en)
CA (1) CA2022842A1 (en)
IE (1) IE902889A1 (en)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6133299A (en) * 1993-02-25 2000-10-17 Warner-Lambert Company Methods for treating neurodegenerative diseases and disorders using N-(2,6-disubstituted aromatic)-N'-pyridinyl ureas and other anticonvulsant compounds
US6329886B1 (en) 1998-05-12 2001-12-11 Nec Corporation Impedance-matching method and circuit at different frequences
KR101303088B1 (en) * 2009-02-17 2013-09-06 한림제약(주) Injectable pharmaceutical composition comprising 3-(hydroxymethyl)-5,5-diphenylhydantoin disodium phosphate ester
CN103288877B (en) * 2013-05-10 2016-03-09 安徽省先锋制药有限公司 Organic amine salt that prophenytoin is stable and its production and use

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4260769A (en) * 1977-04-22 1981-04-07 Interx Research Corporation 5,5-Diphenylhydantoins
EP0011828A1 (en) * 1978-11-23 1980-06-11 The Wellcome Foundation Limited Pharmaceutical combinations including hydantoin derivatives, pharmaceutical formulations containing the combinations and methods of making the formulations
US4925860A (en) * 1987-08-05 1990-05-15 E. I. Du Pont De Nemours And Company Stable pharmaceutical composition of 3-(hydroxymethyl)-5,5-diphenylhydantoin disodium phosphate ester

Also Published As

Publication number Publication date
JP3101305B2 (en) 2000-10-23
JPH03141263A (en) 1991-06-17
EP0427925A3 (en) 1991-07-31
EP0427925A2 (en) 1991-05-22
CA2022842A1 (en) 1991-02-11
AU6083990A (en) 1991-02-14
IE902889A1 (en) 1991-02-27
AU624262B2 (en) 1992-06-04

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